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Stable compositions of fesoterodine

Inactive Publication Date: 2015-07-02
HETERO RES FOUND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent text describes a new pharmaceutical composition that includes fesoterodine fumarate, glyceryl behenate, and a stabilizer. The composition is stable and can be made into a variety of formulations, such as tablets or creams. The technical effect of this invention is that it provides a stable and effective pharmaceutical composition that can be used to treat various medical conditions.

Problems solved by technology

During storage, fesoterodine compositions yields various impurities in variable quantities, which is not desirable if they are beyond certain limits.

Method used

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  • Stable compositions of fesoterodine

Examples

Experimental program
Comparison scheme
Effect test

example-1

Pre-Lubrication of Excipients with Glyceryl Behenate

Fesoterodine Tablets Prepared According to the Composition Listed in Table 2 Using the Following Steps:

[0066]1. Pregelatinized starch, citric acid monohydrate, hydroxypropyl methylcellulose K100 CR, hydroxypropyl methylcellulose K100M CR, hydroxypropyl methylcellulose K4M, and colloidal silicon dioxide were sifted with a half quantity of glyceryl behenate through a mesh #40 sieve and dry blended for 15 minutes.[0067]2. 10% blend of step 1 and fesoterodine hydrogen fumarate were sifted together through a mesh #40 sieve.[0068]3. sifted materials of step 1 and step 2 were blended for 10 minutes.[0069]4. remaining half quantity of glyceryl behenate was sifted through a mesh #60 sieve.[0070]5. blend of step 3 was lubricated with glyceryl behenate of step 4.[0071]6. lubricated blend of step 5 was directly compressed into tablets.[0072]7. tablets of step 6 were film coated using an Opadry® dispersion.

TABLE 2Fesoterodine tablet composition...

example 3-5

[0077]

TABLE 4Fesoterodine tablet compositions prepared by granulation process:Example-3Example-4Example-5mg / Tabletmg / Tabletmg / Tablet(Dry (Wet(WetIngredientsgranulation)granulation)granulation)Intra-granular ingredientsFesoterodine fumarate8.008.008.00Pregelatinized starch147.44147.44147.44Hydroxypropyl72.0072.0072.00methylcelluloseK100 CRHydroxypropyl48.0048.0048.00methylcelluloseK100M CRHydroxypropyl24.0024.0024.00methylcelluloseK4MCitric acid0.660.660.66monohydrateColloidal9.909.909.90silicon dioxideGlyceryl behenate5.005.005.00GranulationPurified water—q.s.—Isopropyl alcohol——q.s.ExtragranularingredientsGlyceryl behenate5.005.005.00Core tablet weight320.0320.0320.0Film coatingOpadry ® blue10.0010.0010.00Film coated tablet weight330.00330.00330.00

Manufacturing Process for Example 3-5:

[0078]1. Pregelatinized starch, citric acid monohydrate, hydroxypropyl methylcellulose K100 CR, hydroxypropyl methylcellulose K100M CR, hydroxypropyl methylcellulose K4M and colloidal silicon dioxide ...

example 6

Fesoterodine Tablet Compositions Prepared by Direct Compression Process

[0082]

Ingredientmg / TabletFesoterodine fumarate8.00Pregelatinized starch116.10Hydroxypropyl72.00methylcellulose K 100 CRHydroxypropyl48.00methylcellulose K 100M CRHydroxypropyl24.00methylcellulose K 4M CRHydroxypropyl cellulose32.00Colloidal silicon dioxide9.90Glyceryl behenate10.00Core tablet weight320.00Film coatingOpadry ® blue10.00Coated tablet weight330.00

Manufacturing Process:

[0083]1. Pregelatinized starch, hydroxypropyl methylcellulose K 100 CR, hydroxypropyl methylcellulose K 100M CR, hydroxypropyl methylcellulose K4M CR, hydroxypropyl cellulose, colloidal silicon dioxide were sifted with a half quantity of glyceryl behenate through a mesh #40 sieve and blended for 15 minutes.

2. 10% of the blend of step 1 and fesoterodine fumarate were sifted together through a mesh #40 sieve.

3. sifted materials of step 1 and 2 were blended for 10 minutes.

4. remaining half quantity of glyceryl behenate was sifted through a...

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Abstract

Stable pharmaceutical compositions of fesoterodine or its pharmaceutically acceptable salt thereof and process for preparing the same. In a first embodiment, a stable pharmaceutical composition is provided comprising fesoterodine fumarate, glyceryl behenate and a stabilizer. The stable pharmaceutical tablet composition may further comprise i) fesoterodine fumarate in an 5 amount of 1% to 5% by weight, ii) glyceryl behenate in an amount of 1% to 8% by weight, iii) pregelatinized starch in an amount of 30% to 50% by weight and iv) a stabilizer in an amount of 0.1% to 10% by weight based on total weight of the composition.

Description

PRIORITY[0001]This patent application claims priority to Indian patent application number 2633 / CHE / 2012, filed on Jul. 2, 2012, the contents of which are incorporated by reference herein in their entirety.FIELD OF THE INVENTION[0002]The present invention encompasses stable pharmaceutical compositions of fesoterodine or pharmaceutically acceptable salts thereof.BACKGROUND OF THE INVENTION[0003]Chemically, fesoterodine fumarate is designated as isobutyric acid 2-((R)-3-diisopropylammonium-1phenylpropyl)-4-(hydroxymethyl) phenyl ester hydrogen fumarate. Its empirical formula is C30H41NO7, corresponding to a molecular weight of 527.66 having the following structural formula:[0004]Fesoterodine is marketed under the trade name TOVIAZ® in United States by Pfizer in the form of 4 mg and 8 mg tablets for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency.[0005]U.S. Pat. No. 6,858,650 and U.S. Pat. No. 7,384,980 disclose fesoterodine.[0006]U...

Claims

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Application Information

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IPC IPC(8): A61K47/36A61K9/20A61K47/14A61K47/38A61K47/12A61K31/195
CPCA61K47/36A61K47/12A61K31/195A61K9/2013A61K47/38A61K9/2059A61K9/2054A61K47/14A61K31/222
Inventor REDDY, BANDI PARTHASARADHIKHADGAPATHI, PODILISYAMPRASAD, BORRA
Owner HETERO RES FOUND
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